RU2345994C2 - МЕЗИЛАТ 4-(4-ТРАНС-ГИДРОКСИЦИКЛОГЕКСИЛ) АМИНО-2-ФЕНИЛ-7Н-ПИРРОЛО[2,3d] ПИРИМИДИНА И ЕГО ПОЛИМОРФНЫЕ ФОРМЫ (ВАРИАНТЫ) - Google Patents

МЕЗИЛАТ 4-(4-ТРАНС-ГИДРОКСИЦИКЛОГЕКСИЛ) АМИНО-2-ФЕНИЛ-7Н-ПИРРОЛО[2,3d] ПИРИМИДИНА И ЕГО ПОЛИМОРФНЫЕ ФОРМЫ (ВАРИАНТЫ) Download PDF

Info

Publication number: RU2345994C2
Authority: RU; Russia
Prior art keywords: hydroxycyclohexyl; pyrrolo; trans; phenyl; amino
Prior art date: 2003-04-22

Application number

RU2005136215/04A

Other languages

English (en)

Russian (ru)

Other versions

RU2005136215A (ru

Inventor

Тимо ХАЙНРИХ (DE)

Тимо ХАЙНРИХ

Аксель ПАЛЬ (DE)

Аксель Паль

Бернд-Мартин ЛЮЙТДЖЕНС (DE)

Бернд-Мартин ЛЮЙТДЖЕНС

Эмиль ФИННЕР (DE)

Эмиль Финнер

Питер К. ВЕРВЕЕР (NL)

Питер К. ВЕРВЕЕР

Ян ЗОРГДРАГЕР (NL)

Ян Зоргдрагер

Original Assignee

Солвей Фармасьютикалс Гмбх

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2003-04-22

Filing date

2004-04-21

Publication date

2009-02-10

2004-04-21 Application filed by Солвей Фармасьютикалс Гмбх filed Critical Солвей Фармасьютикалс Гмбх

2006-03-20 Publication of RU2005136215A publication Critical patent/RU2005136215A/ru

2009-02-10 Application granted granted Critical

2009-02-10 Publication of RU2345994C2 publication Critical patent/RU2345994C2/ru

Links

AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 title claims abstract description 34
150000001875 compounds Chemical class 0.000 claims abstract description 17
239000002253 acid Substances 0.000 claims abstract description 11
206010007559 Cardiac failure congestive Diseases 0.000 claims abstract description 4
206010019280 Heart failures Diseases 0.000 claims abstract description 4
206010020772 Hypertension Diseases 0.000 claims abstract description 4
208000001647 Renal Insufficiency Diseases 0.000 claims abstract description 4
201000006370 kidney failure Diseases 0.000 claims abstract description 4
230000001270 agonistic effect Effects 0.000 claims abstract 2
230000000694 effects Effects 0.000 claims abstract 2
238000000634 powder X-ray diffraction Methods 0.000 claims description 15
238000002844 melting Methods 0.000 claims description 6
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239000008194 pharmaceutical composition Substances 0.000 claims description 3
JAVQQLIFVFPAQG-UHFFFAOYSA-N 2-phenyl-7h-pyrrolo[2,3-d]pyrimidin-4-amine Chemical compound N=1C=2NC=CC=2C(N)=NC=1C1=CC=CC=C1 JAVQQLIFVFPAQG-UHFFFAOYSA-N 0.000 claims 10
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OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 12
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238000000034 method Methods 0.000 description 7
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WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 6
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DSJCRUASBUFVLX-UHFFFAOYSA-N 2-phenyl-7H-pyrrolo[3,2-d]pyrimidin-4-amine Chemical compound NC1=NC(=NC2=C1N=CC2)C1=CC=CC=C1 DSJCRUASBUFVLX-UHFFFAOYSA-N 0.000 description 5
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208000024891 symptom Diseases 0.000 description 2
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KTUQUZJOVNIKNZ-UHFFFAOYSA-N butan-1-ol;hydrate Chemical compound O.CCCCO KTUQUZJOVNIKNZ-UHFFFAOYSA-N 0.000 description 1
235000010216 calcium carbonate Nutrition 0.000 description 1
MIOPJNTWMNEORI-UHFFFAOYSA-N camphorsulfonic acid Chemical compound C1CC2(CS(O)(=O)=O)C(=O)CC1C2(C)C MIOPJNTWMNEORI-UHFFFAOYSA-N 0.000 description 1
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239000003701 inert diluent Substances 0.000 description 1
NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
239000008101 lactose Substances 0.000 description 1
229940057995 liquid paraffin Drugs 0.000 description 1
239000000314 lubricant Substances 0.000 description 1
235000019359 magnesium stearate Nutrition 0.000 description 1
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238000002156 mixing Methods 0.000 description 1
239000012299 nitrogen atmosphere Substances 0.000 description 1
QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
239000003921 oil Substances 0.000 description 1
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239000000546 pharmaceutical excipient Substances 0.000 description 1
NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
239000010452 phosphate Substances 0.000 description 1
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239000010703 silicon Substances 0.000 description 1
229910000029 sodium carbonate Inorganic materials 0.000 description 1
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239000002904 solvent Substances 0.000 description 1
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239000008117 stearic acid Substances 0.000 description 1
150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
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235000012222 talc Nutrition 0.000 description 1
238000012360 testing method Methods 0.000 description 1
GZXOHHPYODFEGO-UHFFFAOYSA-N triglycine sulfate Chemical class NCC(O)=O.NCC(O)=O.NCC(O)=O.OS(O)(=O)=O GZXOHHPYODFEGO-UHFFFAOYSA-N 0.000 description 1
RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
238000001291 vacuum drying Methods 0.000 description 1

Images

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives

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Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Cardiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Life Sciences & Earth Sciences (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Heart & Thoracic Surgery (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Chemical Kinetics & Catalysis (AREA)
Animal Behavior & Ethology (AREA)
General Health & Medical Sciences (AREA)
Public Health (AREA)
Hospice & Palliative Care (AREA)
Urology & Nephrology (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

RU2005136215/04A 2003-04-22 2004-04-21 МЕЗИЛАТ 4-(4-ТРАНС-ГИДРОКСИЦИКЛОГЕКСИЛ) АМИНО-2-ФЕНИЛ-7Н-ПИРРОЛО[2,3d] ПИРИМИДИНА И ЕГО ПОЛИМОРФНЫЕ ФОРМЫ (ВАРИАНТЫ) RU2345994C2 (ru)

Applications Claiming Priority (4)

Application Number	Priority Date	Filing Date
US46442203P	2003-04-22	2003-04-22
EP03101093.7		2003-04-22
EP03101093		2003-04-22
US60/464,422		2003-04-22

Publications (2)

Publication Number	Publication Date
RU2005136215A RU2005136215A (ru)	2006-03-20
RU2345994C2 true RU2345994C2 (ru)	2009-02-10

Family

ID=36143550

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
RU2005136215/04A RU2345994C2 (ru)	2003-04-22	2004-04-21	МЕЗИЛАТ 4-(4-ТРАНС-ГИДРОКСИЦИКЛОГЕКСИЛ) АМИНО-2-ФЕНИЛ-7Н-ПИРРОЛО[2,3d] ПИРИМИДИНА И ЕГО ПОЛИМОРФНЫЕ ФОРМЫ (ВАРИАНТЫ)

Country Status (25)

Country	Link
US (1)	US7381729B2 (uk)
EP (1)	EP1641797B1 (uk)
JP (1)	JP2006524214A (uk)
KR (1)	KR20060021296A (uk)
CN (1)	CN100360533C (uk)
AR (1)	AR043880A1 (uk)
AT (1)	ATE373002T1 (uk)
AU (1)	AU2004232495B2 (uk)
BR (1)	BRPI0409511A (uk)
CA (1)	CA2522810A1 (uk)
DE (1)	DE602004008919T2 (uk)
DK (1)	DK1641797T3 (uk)
ES (1)	ES2290696T3 (uk)
IL (1)	IL171120A (uk)
MX (1)	MXPA05011348A (uk)
NO (1)	NO20055495L (uk)
PL (1)	PL1641797T3 (uk)
PT (1)	PT1641797E (uk)
RU (1)	RU2345994C2 (uk)
SA (1)	SA04250093B1 (uk)
SI (1)	SI1641797T1 (uk)
TW (1)	TWI324517B (uk)
UA (1)	UA81806C2 (uk)
WO (1)	WO2004094428A1 (uk)
ZA (1)	ZA200508519B (uk)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
RU2646599C2 (ru) *	2012-09-27	2018-03-06	Саншайн Лейк Фарма Ко., Лтд	Кристаллические формы производных дигидропиримидина

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Publication number	Priority date	Publication date	Assignee	Title
AR043880A1 (es)	2003-04-22	2005-08-17	Solvay Pharm Gmbh	Mesilato acido de 4-(4.trans-hidroxiciclohexil) amino-2-fenil-7h-pirrolo (2,3-d) pirimidina y sus formas polimorfas
WO2007073855A1 (en) *	2005-12-23	2007-07-05	Bayer Healthcare Ag	Use of adenosine a1 receptor agonists for the protection of renal cells against toxic effects caused by aminoglycosides during treatment of infectious diseases
TW200808819A (en) *	2006-06-19	2008-02-16	Solvay Pharm Gmbh	Use of adenosine A1 antagonists in radiocontrast media induced nephrophaty

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RU2124015C1 (ru) *	1992-12-17	1998-12-27	Пфайзер Инк.	Производные пирроло [2,3-d] пиримидинов, фармацевтическая композиция, пирроло [2,3-d] пиримидины, производные пиррола
WO1999062518A1 (en) *	1998-06-02	1999-12-09	Osi Pharmaceuticals, Inc.	PYRROLO[2,3d]PYRIMIDINE COMPOSITIONS AND THEIR USE

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CS249455B1 (en) *	1985-01-24	1987-03-12	Miroslav Protiva	N-substituted 2-chloro-7-fluoro-10-piperazino-10,11-dihydrodibenzo(b,f)thiepines and their salts and method of their preparation
JP2815691B2 (ja) *	1990-09-20	1998-10-27	麒麟麦酒株式会社	Ｋｒｎ２３９１酸付加塩およびその用途
FR2708604B1 (fr) *	1993-07-30	1995-10-20	Sanofi Elf	Utilisation de dérivés de benzènesulfonyl-indole pour la préparation de médicaments.
JPH08198876A (ja) *	1995-01-30	1996-08-06	Yoshitomi Pharmaceut Ind Ltd	トランス−Ｎ−（１Ｈ−ピラゾロ〔３，４−ｂ〕ピリジン−４−イル）−４−グアニジノメチルシクロヘキサンカルボキサミド・１メタンスルホン酸塩・１水和物
JPH08337584A (ja) *	1995-04-10	1996-12-24	Dai Ichi Seiyaku Co Ltd	縮合六環式アミノ化合物、これを含有する医薬及びその製法
FR2749846B1 (fr) *	1996-06-17	1998-09-11	Pf Medicament	Sel de methanesulfonate d'une arylpiperazine derivee de tryptamine et ses solvates pour usage pharmaceutique
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2004
- 2004-04-19 AR ARP040101306A patent/AR043880A1/es unknown
- 2004-04-20 TW TW093110973A patent/TWI324517B/zh not_active IP Right Cessation
- 2004-04-21 EP EP04728571A patent/EP1641797B1/en not_active Expired - Lifetime
- 2004-04-21 DE DE602004008919T patent/DE602004008919T2/de not_active Expired - Lifetime
- 2004-04-21 AU AU2004232495A patent/AU2004232495B2/en not_active Ceased
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- 2004-04-21 UA UAA200511088A patent/UA81806C2/uk unknown
- 2004-04-21 KR KR1020057019944A patent/KR20060021296A/ko not_active Ceased
- 2004-04-21 PL PL04728571T patent/PL1641797T3/pl unknown
- 2004-04-21 WO PCT/EP2004/050573 patent/WO2004094428A1/en not_active Ceased
- 2004-04-21 AT AT04728571T patent/ATE373002T1/de active
- 2004-04-21 DK DK04728571T patent/DK1641797T3/da active
- 2004-04-21 CN CNB2004800106903A patent/CN100360533C/zh not_active Expired - Fee Related
- 2004-04-21 SI SI200430470T patent/SI1641797T1/sl unknown
- 2004-04-21 RU RU2005136215/04A patent/RU2345994C2/ru not_active IP Right Cessation
- 2004-04-21 CA CA002522810A patent/CA2522810A1/en not_active Abandoned
- 2004-04-21 JP JP2006505565A patent/JP2006524214A/ja active Pending
- 2004-04-21 PT PT04728571T patent/PT1641797E/pt unknown
- 2004-04-21 BR BRPI0409511-1A patent/BRPI0409511A/pt not_active IP Right Cessation
- 2004-04-21 MX MXPA05011348A patent/MXPA05011348A/es active IP Right Grant
- 2004-04-21 US US10/828,650 patent/US7381729B2/en not_active Expired - Fee Related
- 2004-04-22 SA SA4250093A patent/SA04250093B1/ar unknown
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- 2005-09-27 IL IL171120A patent/IL171120A/en not_active IP Right Cessation
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Publication number	Publication date
EP1641797A1 (en)	2006-04-05
EP1641797B1 (en)	2007-09-12
CN1777606A (zh)	2006-05-24
AU2004232495B2 (en)	2010-04-22
SI1641797T1 (sl)	2007-12-31
DE602004008919D1 (de)	2007-10-25
NO20055495D0 (no)	2005-11-21
AR043880A1 (es)	2005-08-17
TWI324517B (en)	2010-05-11
ATE373002T1 (de)	2007-09-15
US20040248912A1 (en)	2004-12-09
JP2006524214A (ja)	2006-10-26
BRPI0409511A (pt)	2006-04-18
TW200505457A (en)	2005-02-16
AU2004232495A1 (en)	2004-11-04
DE602004008919T2 (de)	2008-06-19
PL1641797T3 (pl)	2008-01-31
CA2522810A1 (en)	2004-11-04
US7381729B2 (en)	2008-06-03
IL171120A (en)	2011-01-31
ES2290696T3 (es)	2008-02-16
WO2004094428A1 (en)	2004-11-04
CN100360533C (zh)	2008-01-09
SA04250093B1 (ar)	2008-07-12
ZA200508519B (en)	2007-04-25
HK1089767A1 (en)	2006-12-08
NO20055495L (no)	2006-01-23
UA81806C2 (uk)	2008-02-11
PT1641797E (pt)	2007-12-21
KR20060021296A (ko)	2006-03-07
RU2005136215A (ru)	2006-03-20
MXPA05011348A (es)	2005-11-28
DK1641797T3 (da)	2007-10-29

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RU2345994C2 - МЕЗИЛАТ 4-(4-ТРАНС-ГИДРОКСИЦИКЛОГЕКСИЛ) АМИНО-2-ФЕНИЛ-7Н-ПИРРОЛО[2,3d] ПИРИМИДИНА И ЕГО ПОЛИМОРФНЫЕ ФОРМЫ (ВАРИАНТЫ) - Google Patents

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